Formoterol Fumarate

What it is and how it works

Mechanism of Action Formoterol fumarate is a long-acting, beta 2 -adrenergic receptor agonist (beta 2 -agonist). Inhaled formoterol fumarate acts locally in the lung as a bronchodilator. In vitro studies have shown that formoterol has more than 200-fold greater agonist activity at beta 2 -receptors than at beta 1 -receptors. Although beta 2 -receptors are the predominant adrenergic receptors in bronchial smooth muscle and beta 1 -receptors are the predominant receptors in the heart, there are also beta 2 -receptors in the human heart comprising 10% to 50% of the total betaadrenergic receptors.

Indications

Formoterol fumarate inhalation solution is a long-acting beta 2 -adrenergic agonist (beta 2 -agonist) indicated for: • Long-term, twice daily (morning and evening) administration in the maintenance treatment of bronchoconstriction in patients with chronic obstructive pulmonary disease (COPD), including chronic bronchitis and emphysema. Important limitations of use: • Formoterol fumarate inhalation solution is not indicated to treat acute deteriorations of chronic obstructive pulmonary disease. ( 1.2 , 5.2 ) •Formoterol fumarate inhalation solution is not indicated to treat asthma. Maintenance Treatment of COPD Formoterol fumarate inhalation solution is indicated for the long-term, twice daily (morning and evening) administration in the maintenance treatment of bronchoconstriction in patients with chronic obstructive pulmonary disease (COPD), including chronic bronchitis and emphysema. Important Limitations of Use Formoterol fumarate inhalation solution is not indicated to treat acute deteriorations of chronic obstructive pulmonary disease [ see WARNINGS AND PRECAUTIONS ].

Dosage and administration (summary)

The recommended dose of formoterol fumarate inhalation solution is one 20 mcg unit-dose vial administered twice daily (morning and evening) by nebulization. A total daily dose greater than 40 mcg is not recommended. Formoterol fumarate inhalation solution should be administered by the orally inhaled route via a standard jet nebulizer connected to an air compressor. The safety and efficacy of formoterol fumarate inhalation solution have been established in clinical trials when administered using the PARI-LC Plus® nebulizer (with a facemask or mouthpiece) and the PRONEB® Ultra compressor.

Contraindications

Use of a LABA, including formoterol fumarate inhalation solution, without an inhaled corticosteroid is contraindicated in patients with asthma [ see WARNINGS and PRECAUTIONS ]. Formoterol fumarate inhalation solution is not indicated for the treatment of asthma. • Use of a LABA, including formoterol fumarate, without an inhaled corticosteroid is contraindicated in patients with asthma.

Warnings and precautions

• LABA as monotherapy (without inhaled corticosteroid) for asthma increases the risk of serious asthma-related events. • Do not initiate formoterol fumarate inhalation solution in acutely deteriorating patients. • Do not use for relief of acute symptoms. Concomitant short-acting beta 2 -agonists can be used as needed for acute relief. • Do not exceed the recommended dose. Excessive use of formoterol fumarate inhalation solution or use in conjunction with other medications containing long-acting beta 2 -agonists, can result in clinically significant cardiovascular effects, and may be fatal.

Pregnancy

Pregnancy Risk Summary There are limited available data with formoterol fumarate inhalation solution use in pregnant women to inform a drug-associated risk of adverse developmental outcomes. Beta-agonists may interfere with uterine contractility (see Clinical Considerations).

Storage and supply

Formoterol fumarate inhalation solution, 20 mcg/2 mL is supplied as clear, colorless sterile solution for nebulization in 2.5 mL low-density polyethylene unit dose vials. Each vial is overwrapped in a foil pouch and supplied in cartons as listed below.

Source: Formoterol Fumarate (Formoterol Fumarate) — US FDA prescribing information, 2025-12-23, DailyMed. Summarised and shortened; the full label governs. Iranian registration, indications and labelling may differ.